BIOAVAILABILITY AND METHODS OF ENHANCING BIOAVAILABILITY

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New technology to enhance bioavailability

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BIOAVAILABILITY AND METHODS OF ENHANCING BIOAVAILABILITY:

BIOAVAILABILITY AND METHODS OF ENHANCING BIOAVAILABILITY 1 Presented by SHAHEEN BEGUM Hallticket No:10S91R0035 UNDER THE GUIDANCE OF Associate Professor. Syed Mohammed Kazim Nizam Institute of Pharmacy & Research Centre Deshmukhi (V), Nalgonda. AFFILIATED TO JNTUH.

CAUSES OF LOW BIOAVAILABILITY :

CAUSES OF LOW BIOAVAILABILITY First pass metabolism Poorly water soluble, slowly absorbing oral drugs Insufficient time for absorption in GIT Poor dissolution (highly ionized and polar) Age,stress,disorders,surgery etc Chemical reactions Metabolism by luminal microflora

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Methods of Enhancing Bioavailability:

Methods of Enhancing Bioavailability 1. Enhancement of drug solibulity: a. Micronization b. Nanonization c. SFR d. SFL e. EPAS f. Use of surfactants g. Molecular encapsulation with cyclodextrins h. Eutectic mixtures 5

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2. Enhancement of drug permeability Lipid technologies Ion Pairing Penetration enhancers 3. Enhancement of drug stability Enteric coating Complexation Use of metabolism inhibitors 4. Enhancement of gastrointestinal retention a. GRDDS 6

OPTIZORB TECHNOLOGY:

OPTIZORB TECHNOLOGY 7

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Optizorb ® technology is a combination of ingredients, which work together to speed up the rate at which the paracetamol tablet disintegrates and dissolves in the stomach. contains paracetamol 500mg along with super-disintegrants. The new combination disperses five times faster and is absorbed 37% faster than standard tablets.     8

HOT-MELT EXTRUSION TECHNOLOGY:

HOT-MELT EXTRUSION TECHNOLOGY The development of novel drugs with poor solubility and bioavailability brought the application of HME into the realm of drug-delivery systems. HME involves the application of heat, pressure and agitation through an extrusion channel to mix materials together, and subsequently forcing them out through a die. HME extrusion has been shown to molecularly disperse poorly soluble drugs in a polymer carrier, increasing dissolution rates and bioavailability. 9

ENHANCEMENT OF BIOAVAILABILITY BY INCREASING PERMEABILITY THROUGH PHYSIOLOGICAL BARRIERS:

ENHANCEMENT OF BIOAVAILABILITY BY INCREASING PERMEABILITY THROUGH PHYSIOLOGICAL BARRIERS NANOPARTICLE SYSTEMS WITH CHELATION AGENTS: Increased BBB permeability and lower toxicity Nanoparticles made of natural or artificial polymers ranging in size from about 10–1000 nm and present a possible tool to transport drugs across the BBB The advantages of nanoparticles include reduced drug toxicity, improved biodistribution and therapeutic efficacy The mechanism by which the nanoparticles deliver drugs into the brain may be involved in the preferential absorption of ApoE and/or B. The particles also appear to mimic LDL and interact with the LDL receptor, resulting in their uptake by brain endothelial cells 10

BIOAVAILABILITY ENHANCEMENT BY BBB:

BIOAVAILABILITY ENHANCEMENT BY BBB 11

Fighting Alzheimer's disease with nanotechnology:

Fighting Alzheimer's disease with nanotechnology PLAQUE FORMATION OF FIBRILS BETA AMYLOID PEPTIDES

BREAKING THROUGH TO THE BRAIN, TO DELIVER A CURE FOR PARKINSON’S:

BREAKING THROUGH TO THE BRAIN, TO DELIVER A CURE FOR PARKINSON’S Nanotechnology uses a microscopic “bubble” transport system it enables drugs to traverse the normally uncrossable blood brain barrier. Vesicles are one of the few things in the body that can permeate the BBB, however, pathogens are able to break down the BBB, enabling substances such as bacteria or other toxins to attack parts of the brain The nanovesicles are highly stable and provide a controlled release mechanism TIGHT JUNCTION GLIAL CELLS Nano bubble releasing drug 13

REFERENCES:

REFERENCES D.M. BRAHMANKAR SUNIL B. JAISWAL Biopharmaceutics and pharmacokinetics a Treatise,Second Edition..Page No:345-363 CVS SUBRAHMANYAM. Text book of Biopharmaceutics and pharmacokinetics . shergill http://archive.ispub.com/journal/the-internet-journal-of-aesthetic-and-antiaging-medicine/volume-2-number-1/phytosomes-the-emerging-technology-for-enhancement-of-bioavailability-of-botanicals-and-nutraceuticals Wilson CG, Clarke CP, Starkey YY, Clarke GD. Comparison of a novel fast-dissolving acetaminophen tablet Martin physical pharmacy and pharmaceutical sciences 5 th edition Leon shargel.applied biopharmaceutics and pharmacokinetics Pharmacokinetic and Bioequivalence Study Evaluating a New Paracetamol/Caffeine Formulation in Healthy Human Volunteers Dongzhou J. Liu1 *, Mitchell Kotler1 and Scott Sharples2 1Medical Affairs and New Products Research and Development, GlaxoSmithKline, Parsippany, NJ 07054, USA 2Celerion, 2420 W Baseline Rd, Tempe, AZ 85283, USA 14

REFERENCES:

Wilson CG, Clarke CP, Starkey YY, Clarke GD. Comparison of a novel fast-dissolving acetaminophen tablet Martin physical pharmacy and pharmaceutical sciences 5 th edition Leon shargel.applied biopharmaceutics and pharmacokinetics 4 th Edition. Pharmacokinetic and Bioequivalence Study Evaluating a New Paracetamol/Caffeine Formulation in Healthy Human Volunteers Dongzhou J. Liu1 *, Mitchell Kotler1 and Scott Sharples2 1Medical Affairs and New Products Research and Development, GlaxoSmithKline, Parsippany, NJ 07054, USA 2 Celerion, 2420 W Baseline Rd, Tempe, AZ 85283, USA Milogibaldi, Biopharmaceutics and clinical pharmacokinetics 4 th Edition Page no 146. Venkateshwarlu, Fundamentals of Biopharmaceutics and pharmacokinetics Page no 331. Remington’s Pharmaceuticals sciences volium 1 Page no 1037 Remington’s Pharmaceuticals sciences volium 1 Page no 1041 Robert E Notary, Biopharmaceutics and pharmacokinetics. Indian Journal of Pharmaceutical sciences. 15 REFERENCES

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